HRP20170750T1 - Derivati benzimidazolona kao inhibitori bromodomena - Google Patents
Derivati benzimidazolona kao inhibitori bromodomena Download PDFInfo
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- HRP20170750T1 HRP20170750T1 HRP20170750TT HRP20170750T HRP20170750T1 HR P20170750 T1 HRP20170750 T1 HR P20170750T1 HR P20170750T T HRP20170750T T HR P20170750TT HR P20170750 T HRP20170750 T HR P20170750T HR P20170750 T1 HRP20170750 T1 HR P20170750T1
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- Prior art keywords
- alkyl
- heteroaryl
- cycloalkyl
- aryl
- optionally substituted
- Prior art date
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- 102000001805 Bromodomains Human genes 0.000 title 1
- 108050009021 Bromodomains Proteins 0.000 title 1
- 150000008641 benzimidazolones Chemical class 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 19
- 229910003827 NRaRb Inorganic materials 0.000 claims 18
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 17
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 17
- 229910052736 halogen Inorganic materials 0.000 claims 14
- 150000002367 halogens Chemical class 0.000 claims 14
- 125000000623 heterocyclic group Chemical group 0.000 claims 12
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 10
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 6
- 125000001624 naphthyl group Chemical group 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 5
- 125000000172 C5-C10 aryl group Chemical group 0.000 claims 4
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000001118 alkylidene group Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- -1 -C3- C6 cycloalkyl Chemical group 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 201000006370 kidney failure Diseases 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- GJVFBWCTGUSGDD-UHFFFAOYSA-L pentamethonium bromide Chemical compound [Br-].[Br-].C[N+](C)(C)CCCCC[N+](C)(C)C GJVFBWCTGUSGDD-UHFFFAOYSA-L 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 101150073096 NRAS gene Proteins 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 210000002418 meninge Anatomy 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 210000000664 rectum Anatomy 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epidemiology (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (19)
1. Spoj sa Formulom (I)
[image]
gdje
R1a i R1b su svaki nezavisno C1-C6 alkil, C1-C6 alkoksi, C1-C6 haloalkil, C1-C6 haloalkoksi, C1-C6 hidroksialkil, C3-C6 cikloalkil, ili CH2-C3-C6 cikloalkil;
R2a i R2b su svaki nezavisno H ili halogen;
R3 je
C5-C10 aril, C5-C10 heteroaril, ili C5-C10 heteroarilalkil, od kojih je svaki po izboru supstituiran sa od 1 do 5 R20 grupa; ili
-S(O)2NHR4,
gdje R4 je C1-C6 alkil ili C3-C7 cikloalkil, od kojih je svaki po izboru supstituiran sa od 1 do 5 R20 grupa; ili
segment koji ima formulu
[image]
gdje
R6 je H, OH, ili halogen; i R7 i R8 su svaki nezavisno C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C6 cikloalkil, C1-C6 heteroalkil, C5-C12 aril, C5-C12 heteroaril, ili C5-C12 heteroarilalkil, od kojih je svaki po izboru supstituiran sa od 1 do 5 R20 grupa; ili
R6 je H, C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C6 cikloalkil, fenil, naftil, ili C3-C12 heteroaril; i R7 i R8 zajedno formiraju C1-C6 alkiliden grupu koja ima dvostruku vezu sa ugljikom za koji je svaki od R6, R7, i R8 vezan gdje svaki od C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, -C3-C6 cikloalkil, fenil, naftil, ili C3-C12 heteroaril grupa je po izboru supstituirana sa od 1 do 5 R20 grupa;
X je N-Q, ili O;
Q je H, C1-C3 alkil, C1-C3 haloalkil, benzil ili supstituirani benzil;
svaki R20 je nezavisno C1-C6 alkil, C3-C6 cikloalkil, C1-C6 heteroalkil, C3-C6 heterociklil, C5-C12 aril, C5-C12 heteroaril, halogen, okso, -ORa, -C(O)Ra,-C(O)ORa, -C(O)NRaRb, -OC(O)NRaRb, NRaRb, -NRaC(O)Rb,-NRaC(O)ORb, -S(O)0-2Ra, -S(O)2NRaRb, -NRaS(O)2Rb, -N3, -CN, ili -NO2, gdje svaki C1-C6 alkil, C3-C6 cikloalkil, C1-C6 heteroalkil, C3-C6 heterociklil, C5-C12 aril, C5-C12 heteroaril je po izboru supstituiran sa jednim do pet od halogen, okso, -ORa, -C(O)Ra, -C(O)ORa, -C(O)NRaRb,-OC(O)NRaRb, NRaRb, NRaC(O)Rb, -NRaC(O)ORb, -S(O)0-2Ra,-S(O)2NRaRb, -NRaS(O)2Rb, -N3, -CN, ili NO2;
svaki Ra i Rb je nezavisno H; ili C1-C6 alkil, C3-C6 cikloalkil, C1-C6 heteroalkil, C3-C6 heterociklil, C5-C12 aril, C5-C12 heteroaril, od kojih je svaki po izboru supstituiran sa jednim do pet R21; ili Ra i Rb zajedno sa atomima za koje su vezani formiraju heterocikl, i;
svaki R21 je nezavisno C1-C6 alkil, C3-C6 cikloalkil, C1-C6 heteroalkil, C3-C6 heterociklil, C5-C12 aril, C5-C12 heteroaril, ili halogen;
ili farmaceutski prihvatljiva sol istog.
2. Spoj iz patentnog zahtjeva 1, sa Formulom (Ia)
[image]
gdje
R3 je
C5-C10 aril, C5-C10 heteroaril, ili C5-C10 heteroarilalkil, od kojih je svaki po izboru supstituiran sa od 1 do 5 R20 grupa; ili
-S(O)2NHR4, gdje R4 je C1-C6 alkil ili C3-C7 cikloalkil, od kojih je svaki po izboru supstituiran sa od 1 do 5 R20 grupa; ili
segment koji ima formulu
[image]
gdje
R6 je H, OH, ili halogen; i R7 i R8 su svaki nezavisno C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C6 cikloalkil, C1-C6 heteroalkil, C5-C12 aril, C5-C12 heteroaril, ili C5-C12 heteroarilalkil, od kojih je svaki po izboru supstituiran sa od 1 do 5 R20 grupa; ili
R6 je H, C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C6 cikloalkil, fenil, naftil, ili C3-C12 heteroaril; i R7 i R8 zajedno formiraju C1-C6 alkiliden grupu koja ima dvostruku vezu sa ugljikom za koji svaki od R6, R7, i R8 su vezani gdje svaki od C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, -C3-C6 cikloalkil, fenil, naftil, ili C3-C12 heteroaril grupa je po izboru supstituirana sa od 1 do 5 R20 grupa;
Q je H, C1-C3 alkil, C1-C3 haloalkil, benzil ili supstituirani benzil;
svaki R20 je nezavisno C1-C6 alkil, C3-C6 cikloalkil, C1-C6 heteroalkil, C3-C6 heterociklil, C5-C12 aril, C5-C12 heteroaril, halogen, okso, -ORa, -C(O)Ra,-C(O)ORa, -C(O)NRaRb, -OC(O)NRaRb, NRaRb, -NRaC(O)Rb,-NRaC(O)ORb, -S(O)0-2Ra, -S(O)2NRaRb, NRaS(O)2Rb, -N3, -CN, ili NO2, gdje svaki C1-C6 alkil, C3-C6 cikloalkil, C1-C6 heteroalkil, C3-C6 heterociklil, C5-C12 aril, C5-C12 heteroaril je po izboru supstituiran sa jednim do pet halogen, okso, -ORa, -C(O)Ra, -C(O)ORa, -C(O)NRaRb,-OC(O)NRaRb, -NRaRb, -NRaC(O)Rb, -NRaC(O)ORb, -S(O)0-2Ra,-S(O)2NRaRb, -NRaS(O)2Rb, -N3, -CN, ili -NO2;
svaki Ra i Rb je nezavisno H; ili C1-C6 alkil, C3-C6 cikloalkil, C1-C6 heteroalkil, C3-C6 heterociklil, C5-C12 aril, C5-C12 heteroaril, od kojih je svaki po izboru supstituiran sa jednim do pet R21; ili Ra i Rb zajedno sa atomima za koje su vezani formiraju heterocikl, i;
svaki R21 je nezavisno C1-C6 alkil, C3-C6 cikloalkil, C1-C6 heteroalkil, C3-C6 heterociklil, C5-C12 aril, C5-C12 heteroaril, ili halogen;
ili farmaceutski prihvatljiva sol istog.
3. Spoj iz patentnog zahtjeva 1, sa Formulom (Ib)
[image]
gdje
R3 je
C5-C10 aril, C5-C10 heteroaril, ili C5-C10 heteroarilalkil, od kojih je svaki po izboru supstituiran sa od 1 do 5 R20 grupa; ili
-S(O)2NHR4,
gdje R4 je C1-C6 alkil ili C3-C7 cikloalkil, od kojih je svaki po izboru supstituiran sa od 1 do 5 R20 grupa; ili
segment koji ima formulu
[image]
gdje
R6 je H, OH, ili halogen; i R7 i R8 su svaki nezavisno C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C6 cikloalkil,
C1-C6 heteroalkil, C5-C12 aril, C5-C12 heteroaril, ili C5-C12 heteroarilalkil, od kojih je svaki po izboru supstituiran sa od 1 do 5 R20 grupa; ili
R6 je H, C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C6 cikloalkil, fenil, naftil, ili C3-C12 heteroaril; i R7 i R8 zajedno formiraju a C1-C6 alkiliden grupu koja ima dvostruku vezu sa ugljikom za koji svaki od R6, R7, i R8 su vezani gdje svaki od C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C6 cikloalkil, fenil, naftil, ili C3-C12 heteroaril grupe je po izboru supstituiran sa od 1 do 5 R20 grupa;
svaki R20 je nezavisno C1-C6 alkil, C3-C6 cikloalkil, C1-C6 heteroalkil, C3-C6 heterociklil, C5-C12 aril, C5-C12 heteroaril, halogen, okso, -ORa, -C(O)Ra,-C(O)ORa, -C(O)NRaRb, -OC(O)NRaRb, -NRaRb, NRaC(O)Rb,-NRaC(O)ORb, -S(O)0-2Ra, -S(O)2NRaRb, -NRaS(O)2Rb, -N3, -CN, ili NO2, gdje svaki C1-C6 alkil, C3-C6 cikloalkil, C1-C6 heteroalkil, C3-C6 heterociklil, C5-C12 aril, C5-C12 heteroaril je po izboru supstituiran sa od jednim do pet halogen, okso, -ORa, -C(O)Ra, -C(O)ORa, -C(O)NRaRb,-OC(O)NRaRb, -NRaRb, -NRaC(O)Rb, -NRaC(O)ORb, -S(O)0-2Ra,-S(O)2NRaRb, -NRaS(O)2Rb, -N3, -CN, ili NO2;
svaki Ra i Rb je nezavisno H; ili C1-C6 alkil, C3-C6 cikloalkil, C1-C6 heteroalkil, C3-C6 heterociklil, C5-C12 aril, C5-C12 heteroaril, od kojih je svaki po izboru supstituiran sa jednim do pet R21; ili Ra i Rb zajedno sa atomima za koje su vezani formiraju heterocikl, i;
svaki R21 je nezavisno C1-C6 alkil, C3-C6 cikloalkil, C1-C6 heteroalkil, C3-C6 heterociklil, C5-C12 aril, C5-C12 heteroaril, ili halogen;
ili farmaceutski prihvatljiva sol istog.
4. Spoj iz bilo kojeg od patentnih zahtjeva 1-3, gdje R3 je C5-C10 aril, C5-C10 heteroaril, ili C5-C10 heteroarilalkil, od kojih je svaki po izboru supstituiran sa od 1 do 5 R20 grupa.
5. Spoj iz bilo kojeg od patentnih zahtjeva 1-3, gdje R3 je segment koji ima formulu
[image]
gdje R6 je H, OH, ili halogen; i
R7 i R8 su svaki nezavisno C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C6 cikloalkil, C1-C6 heteroalkil, C5-C12 aril, C5-C12 heteroaril, ili C5-C12 heteroarilalkil, od kojih je svaki po izboru supstituiran sa od 1 do 5 R20 grupa.
6. Spoj iz patentnog zahtjeva 5, gdje R6 je OH.
7. Spoj iz patentnog zahtjeva 5, gdje R7 i R8 su svaki nezavisno C1-C6 alkil, C3-C6 cikloalkil, C1-C6 heteroalkil, C5-C12 aril, C5-C12 heteroaril, ili C5-C12 heteroarilalkil, od kojih je svaki po izboru supstituiran sa od 1 do 5 R20 grupa.
8. Spoj iz patentnog zahtjeva 5, gdje R7 i R8 su svaki nezavisno C1-C6 alkil, C6 aril ili C6 heteroaril, od kojih je svaki po izboru supstituiran sa od 1 do 5 R20 grupa.
9. Spoj iz patentnog zahtjeva 5, gdje R7 i R8 su svaki nezavisno C6 aril ili C6 heteroaril, od kojih je svaki po izboru supstituiran sa od 1 do 5 R20 grupa.
10. Spoj iz patentnog zahtjeva 5, gdje R7 i R8 su svaki nezavisno C1-C6 alkil, od kojih je svaki po izboru supstituiran sa od 1 do 5 R20 grupa.
11. Spoj iz patentnog zahtjeva 1 izabrano sa sljedeće liste:
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12. Spoj iz patentnog zahtjeva 1 izabrano sa sljedeće liste:
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i
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13. Farmaceutska kompozicija koja sadrži spoj iz bilo kojeg od patentnih zahtjeva 1-12, ili njegovu farmaceutski prihvatljivu sol, i farmaceutski prihvatljiv nosač.
14. Spoj iz bilo kojeg od patentnih zahtjeva 1-12 za primjenu u liječenju čovjeka koji ima bolest ili stanje koje je autoimuna bolest, inflamatorna bolest, neurodegenerativna bolest, rak, kardiovaskularni poremećaj, poremećaj bubrega, virusna infekcija, ili pretilost.
15. Primjena spoja iz bilo kojeg od patentnih zahtjeva 1-12 za proizvodnju lijeka za liječenje čovjeka koji ima stanje ili bolest koje je autoimuna bolest, inflamatorna bolest, neurodegenerativna bolest, rak, kardiovaskularni poremećaj, poremećaj bubrega, virusna infekcija, ili pretilost.
16. Spoj za primjenu prema patentnom zahtjevu 14 ili primjenu prema patentnom zahtjevu 15, gdje bolest ili stanje je solidni tumor debelog crijeva, rektuma, prostate, pluća, gušterače, jetre, bubrega, cerviksa, želuca, jajnika, dojke, kože, mozga, moždanih ovojnica, ili centralnog živčanog sustava.
17. Spoj za primjenu prema patentnom zahtjevu 14 ili primjenu prema patentnom zahtjevu 15, gdje bolest ili stanje je multipli mijelom.
18. Spoj za primjenu prema patentnom zahtjevu 14 ili primjenu prema patentnom zahtjevu 15, gdje bolest ili stanje je B-stanični limfom.
19. Spoj za primjenu prema patentnom zahtjevu 14 ili primjenu prema patentnom zahtjevu 15, gdje bolest ili stanje je difuzni krupnostanični B-limfom ili Burkitov limfom.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361805995P | 2013-03-28 | 2013-03-28 | |
| US201361860230P | 2013-07-30 | 2013-07-30 | |
| EP14729114.0A EP2978759B1 (en) | 2013-03-28 | 2014-03-27 | Benzimidazolone derivatives as bromodomain inhibitors |
| PCT/US2014/032031 WO2014160873A1 (en) | 2013-03-28 | 2014-03-27 | Benzimidazolone derivatives as bromodomain inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20170750T1 true HRP20170750T1 (hr) | 2017-07-28 |
Family
ID=50897885
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20170750TT HRP20170750T1 (hr) | 2013-03-28 | 2017-05-19 | Derivati benzimidazolona kao inhibitori bromodomena |
Country Status (35)
| Country | Link |
|---|---|
| US (2) | US20160031868A1 (hr) |
| EP (1) | EP2978759B1 (hr) |
| JP (1) | JP6339175B2 (hr) |
| KR (1) | KR101847698B1 (hr) |
| CN (1) | CN105102453B (hr) |
| AP (1) | AP2015008741A0 (hr) |
| AU (1) | AU2014241152B2 (hr) |
| BR (1) | BR112015024078A2 (hr) |
| CA (1) | CA2907502C (hr) |
| CL (1) | CL2015002871A1 (hr) |
| CR (1) | CR20150515A (hr) |
| CY (1) | CY1119165T1 (hr) |
| DK (1) | DK2978759T3 (hr) |
| EA (1) | EA029497B1 (hr) |
| ES (1) | ES2626397T3 (hr) |
| HK (1) | HK1220692A1 (hr) |
| HR (1) | HRP20170750T1 (hr) |
| HU (1) | HUE034772T2 (hr) |
| IL (1) | IL241186A0 (hr) |
| LT (1) | LT2978759T (hr) |
| MD (1) | MD4531C1 (hr) |
| MX (1) | MX2015013798A (hr) |
| MY (1) | MY176634A (hr) |
| NZ (1) | NZ711586A (hr) |
| PE (1) | PE20151982A1 (hr) |
| PH (1) | PH12015502246A1 (hr) |
| PL (1) | PL2978759T3 (hr) |
| PT (1) | PT2978759T (hr) |
| RS (1) | RS56050B1 (hr) |
| SG (1) | SG11201507926RA (hr) |
| SI (1) | SI2978759T1 (hr) |
| TW (1) | TWI530499B (hr) |
| UY (1) | UY35516A (hr) |
| WO (1) | WO2014160873A1 (hr) |
| ZA (1) | ZA201506356B (hr) |
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| JP6599852B2 (ja) | 2013-06-21 | 2019-10-30 | ゼニス・エピジェネティクス・リミテッド | ブロモドメイン阻害剤としての新規の置換された二環式化合物 |
| JP2016523964A (ja) | 2013-07-08 | 2016-08-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｂｅｔタンパク質阻害剤としての三環式複素環 |
| CN105593224B (zh) | 2013-07-31 | 2021-05-25 | 恒元生物医药科技(苏州)有限公司 | 作为溴结构域抑制剂的新型喹唑啉酮类化合物 |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
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| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| LT3134403T (lt) | 2014-04-23 | 2020-05-11 | Incyte Corporation | 1h-pirolo[2,3-c]piridin-7(6h)-onai ir pirazolo[3,4-c]piridin-7(6h)-onai, kaip bet baltymų inhibitoriai |
| US9527864B2 (en) | 2014-09-15 | 2016-12-27 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| WO2016061144A1 (en) | 2014-10-14 | 2016-04-21 | The Regents Of The University Of California | Use of cdk9 and brd4 inhibitors to inhibit inflammation |
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| US10179125B2 (en) | 2014-12-01 | 2019-01-15 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| JP2017537946A (ja) | 2014-12-11 | 2017-12-21 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメイン阻害剤としての置換複素環 |
| CA2966450A1 (en) | 2014-12-17 | 2016-06-23 | Olesya KHARENKO | Inhibitors of bromodomains |
| CA2977308A1 (en) | 2015-03-13 | 2016-09-22 | Resverlogix Corp. | Compositions and therapeutic methods for the treatment of complement-associated diseases |
| GB201504689D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
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| EP3397640B1 (en) | 2015-12-29 | 2021-08-04 | INSERM - Institut National de la Santé et de la Recherche Médicale | Xanthine derivative inhibitors of bet proteins |
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| CN111712496B (zh) | 2017-12-20 | 2023-05-02 | 贝达药业股份有限公司 | 作为溴结构域蛋白质抑制剂的化合物和组合物 |
| CN113365699B (zh) * | 2019-02-02 | 2024-06-14 | 石药集团中奇制药技术（石家庄）有限公司 | 靶向泛素化降解brd4蛋白化合物及其制备方法和应用 |
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